4-[[6-(1,3-benzoxazol-5-ylmethylcarbamoyl)-4-oxo-1H-quinolin-3-yl]methyl]benzoic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 4-[[6-(1,3-benzoxazol-5-ylmethylcarbamoyl)-4-oxo-1H-quinolin-3-yl]methyl]benzoic acid
• 化学式: C₂₆H₁₉N₃O₅
• 分子量: 453.4
• InChiKey: FGOCOMYCVPWXMB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  34
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  122
• 氢给体数：
  3
• 氢受体数：
  7

文献信息

• Naphthalene derivatives as matrix metalloproteinase inhibitors
  申请人：——

  公开号：US20040043983A1

  公开（公告）日：2004-03-04

  This invention provides compounds defined by Formula I 1 or a pharmaceutically acceptable salt thereof, wherein R 1 , Q, Y 3 , Y 4 , U 5 , U 6 , U 8 , R 2 , and R 3 are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MMP-13 enzyme in an animal, comprising administering to the animal a compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP-13 enzyme in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides methods of treating diseases such as heart disease, multiple sclerosis, osteo- and rheumatoid arthritis, arthritis other than osteo- or rheumatoid arthritis, cardiac insufficiency, inflammatory bowel disease, heart failure, age-related macular degeneration, chronic obstructive pulmonary disease, asthma, periodontal diseases, psoriasis, atherosclerosis, and osteoporosis in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides combinations, comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, together with another pharmaceutically active component as described in the specification.

  本发明提供了由公式I1定义的化合物或其药学上可接受的盐，其中R1、Q、Y3、Y4、U5、U6、U8、R2和R3如规范中所定义。本发明还提供了药物组合物，包括公式I中定义的化合物或其药学上可接受的盐，以及药学上可接受的载体、稀释剂或赋形剂。本发明还提供了抑制动物中MMP-13酶的方法，包括向动物内部给予公式I中定义的化合物或其药学上可接受的盐。本发明还提供了治疗由MMP-13酶介导的疾病的方法，包括向患者内部给予公式I中定义的化合物或其药学上可接受的盐，单独使用或与药物组合物一起使用。本发明还提供了治疗心脏病、多发性硬化症、骨关节炎和类风湿性关节炎、非骨关节炎或类风湿性关节炎的关节炎、心力衰竭、炎症性肠病、老年性黄斑变性、慢性阻塞性肺疾病、哮喘、牙周疾病、银屑病、动脉硬化和骨质疏松症的方法，包括向患者内部给予公式I中定义的化合物或其药学上可接受的盐，单独使用或与药物组合物一起使用。本发明还提供了组合物，包括公式I中定义的化合物或其药学上可接受的盐，以及规范中描述的另一种药学活性成分。
• 4-HYDROXYQUINOLINE DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS
  申请人：Warner-Lambert Company LLC

  公开号：EP1539163A1

  公开（公告）日：2005-06-15
• [EN] 4-HYDROXYQUINOLINE DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS<br/>[FR] DERIVES DE 4-HYDROXYQUINOLEINE UTILISES COMME INHIBITEURS DE METALLOPROTEASES MATRICIELLES
  申请人：WARNER LAMBERT CO

  公开号：WO2004014377A1

  公开（公告）日：2004-02-19

  This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R1, Q, Y3, Y4, U5, U6, U8, R2, and R3 are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a pharmaceutically 10 acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an N4MP-13 enzyme in an animal, comprising administering to the animal a compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP 13 enzyme in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides methods of treating diseases such as heart disease, multiple sclerosis, osteo- and rheumatoid arthritis, arthritis other than osteo- or rheumatoid arthritis, cardiac insufficiency, inflammatory bowel disease, heart failure, age-related macular degeneration, chronic obstructive pulmonary disease, asthma, periodontal diseases, psoriasis, atherosclerosis, and osteoporosis in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides combinations, comprising a compound of Formula I, or a pharmaceutically 25 acceptable salt thereof, together with another pharmaceutically active component as described in the specification.